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1. 发明授权

US09266863B2 Process for the synthesis of azacitidine and decitabine 有权
标题翻译：合成阿扎胞苷和地西他滨的方法
公开(公告)号：US09266863B2
公开(公告)日：2016-02-23
申请号：US13073014
申请日：2011-03-28
申请人： Lorenzo De Ferra , Maurizio Zenoni , Stefano Turchetta , Mauro Anibaldi , Ettore Ammirati , Paolo Brandi , Giorgio Berardi
发明人： Lorenzo De Ferra , Maurizio Zenoni , Stefano Turchetta , Mauro Anibaldi , Ettore Ammirati , Paolo Brandi , Giorgio Berardi
IPC分类号： C07H19/12 , C07H1/00 , C07D405/04
CPC分类号： C07D405/04 , C07H1/00 , C07H19/12
摘要： Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.
摘要翻译：本文描述的是在N，O-双 - 三甲基甲硅烷基 - 三氟乙酰胺的存在下合成氮杂胞苷或地西他滨的方法，其包括氮代胞嘧啶的甲硅烷基化。这种反应在有机溶剂中进行，优选非质子性，甚至更优选选自二氯甲烷，二氯乙烷和/或乙腈。根据该方法的另一方面，每摩尔氮杂胞嘧啶使用2至3摩尔N，O-双 - 三甲基甲硅烷基 - 三氟乙酰胺，优选2.2至2.5。

2. 发明申请

US20110245485A1 PROCESS FOR THE SYNTHESIS OF AZACITIDINE AND DECITABINE 有权
标题翻译：合成方法和化合物的方法
公开(公告)号：US20110245485A1
公开(公告)日：2011-10-06
申请号：US13073014
申请日：2011-03-28
申请人： Lorenzo DE FERRA , Maurizio ZENONI , Stefano TURCHETTA , Mauro ANIBALDI , Ettore AMMIRATI , Paolo BRANDI , Giorgio BERARDI
发明人： Lorenzo DE FERRA , Maurizio ZENONI , Stefano TURCHETTA , Mauro ANIBALDI , Ettore AMMIRATI , Paolo BRANDI , Giorgio BERARDI
IPC分类号： C07H19/12 , C07F7/18
CPC分类号： C07D405/04 , C07H1/00 , C07H19/12
摘要： Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.
摘要翻译：本文描述的是在N，O-双 - 三甲基甲硅烷基 - 三氟乙酰胺的存在下合成氮杂胞苷或地西他滨的方法，其包括氮代胞嘧啶的甲硅烷基化。这种反应在有机溶剂中进行，优选非质子性，甚至更优选选自二氯甲烷，二氯乙烷和/或乙腈。根据该方法的另一方面，每摩尔氮杂胞嘧啶使用2至3摩尔N，O-双 - 三甲基甲硅烷基 - 三氟乙酰胺，优选2.2至2.5。

3. 发明申请

US20110111469A1 PROCESS FOR THE PRODUCTION OF N-ACYL-PHOSPHATIDYL-ETHANOLAMINE 有权
标题翻译：制备N-乙酰基 - 苯乙胺的方法
公开(公告)号：US20110111469A1
公开(公告)日：2011-05-12
申请号：US13002693
申请日：2008-07-08
申请人： Lorenzo De Ferra , Mauro Anibaldi , Ettore Ammirati
发明人： Lorenzo De Ferra , Mauro Anibaldi , Ettore Ammirati
IPC分类号： C12P13/00
CPC分类号： C07F9/106 , C07F9/10
摘要： The document describes a process for the preparation of N-Acyl-Phosphatidyl-Ethanolamine of formula (I) on an industrial scale, In which R1, R2 and R3 are, independently from each other, saturated, monounsaturated or polyunsaturated acyls C10-C30, pure or mixed together, and X=OH or OM, where M=alkaline metal or alkaline earth, ammonium or alkylammonium. The process in question allows the conversion of lecithin of synthetic or natural origin into N-Acyl-Phosphatidyl-Ethanolamine of formula (I) of high purity, using a limited molar excess of the reagent N-acyl-ethanolamine, where the acyl is as defined above for the formula (I) through reaction of transphosphatidylation in the presence of the enzyme phospholipase D and in conditions suitable for production on an industrial scale.
摘要翻译：该文献描述了以工业规模制备式（I）的N-酰基 - 磷酰基 - 乙醇胺的方法，其中R 1，R 2和R 3彼此独立地是饱和的，单不饱和或多不饱和酰基C10-C30，纯或混合在一起，X = OH或OM，其中M =碱金属或碱土金属，铵或烷基铵。所讨论的方法允许使用有限摩尔过量的试剂N-酰基 - 乙醇胺将合成或天然来源的卵磷脂转化为高纯度的式（I）的N-酰基 - 磷酰基 - 乙醇胺，其中酰基如通过在磷脂酶D存在下的磷脂酰化反应和适合于工业规模生产的条件下，通式（I）所定义。

4. 发明授权

US08377662B2 Process for the production of N-acyl-phosphatidyl-ethanolamine 有权
标题翻译：制备N-酰基 - 磷脂酰乙醇胺的方法
公开(公告)号：US08377662B2
公开(公告)日：2013-02-19
申请号：US13002693
申请日：2008-07-08
申请人： Lorenzo De Ferra , Mauro Anibaldi , Ettore Ammirati
发明人： Lorenzo De Ferra , Mauro Anibaldi , Ettore Ammirati
IPC分类号： C12P13/00
CPC分类号： C07F9/106 , C07F9/10
摘要： The document describes a process for the preparation of N-Acyl-Phosphatidyl-Ethanolamine of formula (I) on an industrial scale, In which R1, R2 and R3 are, independently from each other, saturated, monounsaturated or polyunsaturated acyls C10-C30, pure or mixed together, and X═OH or OM, where M=alkaline metal or alkaline earth, ammonium or alkylammonium. The process in question allows the conversion of lecithin of synthetic or natural origin into N-Acyl-Phosphatidyl-Ethanolamine of formula (I) of high purity, using a limited molar excess of the reagent N-acyl-ethanolamine, where the acyl is as defined above for the formula (I) through reaction of transphosphatidylation in the presence of the enzyme phospholipase D and in conditions suitable for production on an industrial scale.
摘要翻译：该文献描述了以工业规模制备式（I）的N-酰基 - 磷酰基 - 乙醇胺的方法，其中R 1，R 2和R 3彼此独立地是饱和的，单不饱和或多不饱和酰基C10-C30，纯或混合在一起，X = OH或OM，其中M =碱金属或碱土金属，铵或烷基铵。所讨论的方法允许使用有限摩尔过量的试剂N-酰基 - 乙醇胺将合成或天然来源的卵磷脂转化为高纯度的式（I）的N-酰基 - 磷酰基 - 乙醇胺，其中酰基如通过在磷脂酶D存在下的磷脂酰化反应和适合于工业规模生产的条件下，通式（I）所定义。

5. 发明申请

US20070049637A1 Process for the synthesis of cationic lipids 审中-公开
标题翻译：阳离子脂质合成方法
公开(公告)号：US20070049637A1
公开(公告)日：2007-03-01
申请号：US10579223
申请日：2004-11-03
申请人： Lorenzo De Ferra , Mauro Anibaldi , Ettore Ammirati
发明人： Lorenzo De Ferra , Mauro Anibaldi , Ettore Ammirati
IPC分类号： A61K31/22 , C07C229/02
CPC分类号： C07C213/00 , C07C213/08 , C07C215/10 , C07C219/08 , Y02P20/55
摘要： A process for the synthesis of lipid cations having general formula (6): in which: R1 represents a lipophilic chain; R2, R3, R4, which are identical or different from one another, represent C1-C10 alkyl, C1-C10 alkenyl, or C1-C10 alkynyl radicals, optionally containing hydroxyl, ether, halogen and acyloxy functions, and X− is an oxy-anion or a halide; in which a compound of formula (2), in which R5 and R6, which are identical or different from one another, represent a C1-C5 acyl, a benzyl group or a diol-protective group, is reacted in an alcoholic solvent with from 1 to 6 equivalents of NR2R3R4.
摘要翻译：用于合成具有通式（6）的脂质阳离子的方法：其中：R 1表示亲脂链; R 2，R 3，R 4，它们彼此相同或不同，表示C 1〜 C 1 -C 10烷基，C 1 -C 10链烯基或C 1 -C 10烷基，C 1 -C 10 - 任选地含有羟基，醚，卤素和酰氧基官能团的炔基，X - 是氧阴离子或卤化物; 其中式（2）的化合物（其中R 5和R 6）彼此相同或不同，表示C 1〜 C 1 -C 5酰基，苄基或二醇保护基在醇溶剂中与1至6当量的NR 2 R 2 - 3 R 4。

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